Akt

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  1. pan-Akt inhibitor

    Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5/18/8 nM, 620-fold selectivity over PKA.
  2. Akt inhibitor

    PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
  3. Akt inhibitor

    API-1 (NSC 177223) is a potent inhibitor of Akt that induces GSK3-dependent, β-TrCP- and FBXW7-mediated Mcl-1 degradation, resulting in induction of apoptosis.
  4. NF-κB inhibitor

    Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B is also a regulator of skeletal muscle mass.
  5. flavonoid

    Loureirin A is a flavonoid extracted from Dragon's Blood, can inhibit Akt phosphorylation, and has antiplatelet activity.
  6. Akt inhibitor

    Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively.
  7. anti-tumor agent

    Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory.
  8. anti-inflammatory agent

    Rotundic acid, a triterpenoid obtained from I. rotunda, induces DNA damage and cell apoptosis in hepatocellular carcinoma through AKT/mTOR and MAPK Pathways. Rotundic acid possesses anti-inflammatory and cardio-protective abilities.
  9. Lipoteichoic acid is an orally active compound with anti-inflammatory and antitumor properties. It is a key immune molecule found in Gram-positive bacteria that activates the complement system by upregulating C3 and inhibiting CD55. Lipoteichoic acid modulates macrophage autophagy via the PI3K/Akt/mTOR pathway, induces lung injury in mouse models, and inhibits melanin production.
  10. 6-Demethoxytangeretin is a flavonoid compound isolated from *Citrus reticulata* with demonstrated anti-inflammatory and anti-allergic properties. It inhibits IL-6 production and the expression of related genes in human mast cells by modulating the ALK and MAPK signaling pathways. Additionally, 6-Demethoxytangeretin enhances CRE-mediated transcription in hippocampal neurons, indicating potential neuroregulatory effects.
  11. fMLP inhibitor

    Larixol is an fMLP inhibitor that also suppresses key signaling pathways involved in immune regulation, including Src kinase, ERK1/2, p38, and AKT phosphorylation. It disrupts the interaction between the βγ subunit of the fMLP receptor Gi protein and downstream effectors, thereby inhibiting fMLP-induced respiratory burst. Larixol effectively inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and neutrophil chemotaxis. It mitigates neutrophil hyperactivation and helps reduce inflammation and tissue damage. Additionally, Larixol derivatives have shown inhibitory activity against TRPC6 functional mutants associated with focal segmental glomerulosclerosis (FSGS).
  12. PI3K/Akt/mTOR inhibitor

    PI3K/Akt/mTOR-IN-2 is an inhibitor of the PI3K/AKT/mTOR signaling pathway with demonstrated anticancer activity. It selectively inhibits the proliferation of MDA-MB-231 cells with an IC50 of 2.29 μM and induces cell cycle arrest and apoptosis, making it a promising candidate for cancer research.
  13. PGAM1 inhibitor

    HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1) that induces apoptosis and suppresses cell migration by inhibiting the formation of invasive pseudopodia. It increases oxidative stress, activates the JNK/c-Jun pathway, and downregulates AKT and ERK signaling. HKB99 is a promising compound for the study of non-small cell lung cancer (NSCLC).
  14. ALK/ROS1 inhibitor

    Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor that effectively blocks tyrosine autophosphorylation of ALK, mutant ALK, and EGFR, with IC50 values ranging from 5.38 to 16.74 nM. Additionally, it inhibits the transport activity of MATE1, MATE2K, P-gp, and BCRP. Iruplinalkib is under investigation for the treatment of non-small cell lung cancer (NSCLC).
  15. Endoplasmic Reticulum Stress Inhibitor

    Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects.
  16. TrkA agonist

    Gambogic amide is a potent and selective TrkA agonist that induces tyrosine phosphorylation of TrkA and activates downstream signaling pathways, including Akt and MAPK. It specifically binds to the cytoplasmic juxtamembrane domain of TrkA, promoting receptor dimerization and activation. Gambogic amide exhibits neuroprotective effects by preventing glutamate-induced neuronal cell death and demonstrates improved efficacy in a transient middle cerebral artery occlusion (MCAO) model of stroke, supporting its potential use in research on neurodegenerative diseases and stroke.
  17. mGluR5 allosteric modulator

    CDPPB is a selective, orally active allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). It enhances AKT and ERK1/2 signaling and upregulates BDNF mRNA expression. CDPPB also inhibits caspase-3 activation and mitigates mitochondrial dysfunction, demonstrating therapeutic potential in improving cognitive impairment, depression, and Huntington’s disease.
  18. Hsp90/HSV inhibitor

    AT-533 is a potent inhibitor of heat shock protein 90 (Hsp90) and herpes simplex virus (HSV), exhibiting strong antitumor and antiviral activities. It suppresses tumor growth and angiogenesis by disrupting the HIF-1α/VEGF/VEGFR-2 signaling axis, a critical pathway in tumor vascularization and progression. Additionally, AT-533 inhibits key downstream signaling cascades, including Akt/mTOR/p70S6K, ERK1/2, and FAK pathways. In endothelial cells, specifically human umbilical vein endothelial cells (HUVECs), AT-533 effectively inhibits tube formation, cell migration, and invasion, highlighting its anti-angiogenic properties. These combined effects position AT-533 as a promising candidate for cancer therapy and angiogenesis-related disease research.
  19. Anticholinergic agent

    Penehyclidine hydrochloride (also known as Penequinine hydrochloride) is a selective anticholinergic agent that acts as an antagonist of muscarinic M1 and M3 receptors. It exerts anti-inflammatory effects by modulating immune signaling in lung tissue, notably through activation of the NF-κB pathway and inhibition of pro-inflammatory cytokine release. In preclinical studies, Penehyclidine hydrochloride has been shown to alleviate pulmonary inflammation in rat models of chronic obstructive pulmonary disease (COPD), particularly under conditions of mechanical ventilation. These properties suggest its potential utility in managing respiratory inflammatory conditions and improving outcomes in mechanically ventilated patients with COPD.
  20. Deltonin is a steroidal saponin isolated from *Dioscorea zingiberensis*, exhibiting notable antitumor activity. It exerts its effects by inhibiting the activation of key survival and proliferation pathways, specifically ERK1/2 and AKT signaling. Through this dual inhibition, Deltonin suppresses tumor cell growth and promotes apoptosis, making it a promising candidate for further investigation in cancer research and therapeutic development.
  21. 6-Hydroxyflavone is an orally active flavonoid with diverse pharmacological properties. It exhibits anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-induced nitric oxide (NO) production and also promotes osteoblast differentiation through activation of the AKT, ERK1/2, and JNK signaling pathways, supporting its role in bone health. Additionally, 6-Hydroxyflavone inhibits the glycosylation of bovine hemoglobin (BHb), suggesting potential in managing glycation-related complications. It demonstrates kidney-protective effects and modulates GABAergic neurotransmission by enhancing GABA-induced currents via the benzodiazepine binding sites on GABAA receptors
  22. EGFR activator

    Isoprocurcumenol is a guaiane-type sesquiterpene isolated from *Curcuma comosa* with notable bioactivity in epidermal growth factor receptor (EGFR) signaling. It activates EGFR and enhances downstream phosphorylation of ERK and AKT, key mediators of cell survival and proliferation pathways. As a result, isoprocurcumenol promotes keratinocyte proliferation, suggesting potential applications in skin regeneration, wound healing, and dermatological research.
  23. BMP receptor agonist

    SY-LB-35 is a potent agonist of bone morphogenetic protein (BMP) receptors, capable of activating both canonical and non-canonical signaling pathways. In the C2C12 myoblast cell line, SY-LB-35 significantly enhances cell proliferation and viability, promoting cell cycle progression by increasing the proportion of cells in the S and G2/M phases. Mechanistically, it activates the canonical Smad pathway as well as non-canonical PI3K/Akt, ERK, p38, and JNK signaling cascades. These properties make SY-LB-35 a valuable tool for studying BMP-related cellular processes and a potential therapeutic candidate for tissue regeneration and muscle repair.
  24. PROTAC AKT degrader

    INY-05-040 is a potent and selective PROTAC degrader targeting all three isoforms of AKT (AKT1, AKT2, and AKT3). It induces rapid proteasomal degradation of AKT, effectively inhibiting downstream signaling pathways such as PI3K/AKT/mTOR, which are critical for cancer cell survival and proliferation. INY-05-040 demonstrates broad antiproliferative activity across 288 cancer cell lines, highlighting its potential as a powerful therapeutic agent for targeting AKT-driven malignancies.
  25. AKT PROTAC degrader

    MS15 TFA is a potent and selective PROTAC degrader targeting AKT isoforms. It inhibits the activity of AKT1, AKT2, and AKT3 with IC₅₀ values of 798 nM, 90 nM, and 544 nM, respectively. MS15 TFA serves as a valuable tool for studying AKT signaling and its role in cancer and metabolic diseases.
  26. PROTAC Akt Degrader

    INY-03-041 is a potent and highly selective PROTAC-based pan-AKT degrader that targets AKT1, AKT2, and AKT3 with IC₅₀ values of 2.0 nM, 6.8 nM, and 3.5 nM, respectively. It is composed of the ATP-competitive AKT inhibitor GDC-0068 linked to the cereblon ligand lenalidomide, making it a valuable tool for studying AKT signaling and targeted cancer therapy.
  27. PI3K/Akt/mTOR Inhibitor

    Veratramine is a selective inhibitor of the PI3K/Akt/mTOR signaling pathway and serves as a modulator of SIGMAR1. This compound facilitates autophagic apoptosis in tumor cells, effectively induces G0/G1 cell cycle arrest, and diminishes epithelial-mesenchymal transition (EMT) markers, thereby reducing tumor migration. Additionally, Veratramine exhibits neuroprotective effects by inhibiting SIGMAR1 interactions with NMDAR and the phosphorylation of NMDAR Ser896, resulting in reduced neurological damage in neuropathy models. Its diverse biological activities make it suitable for research on liver cancer, osteosarcoma, and diabetic peripheral neuropathy.
  28. PI3K/Akt/CREB Activator

    PI3K/Akt/CREB activator 1 is a potent, orally active compound that stimulates the PI3K/Akt/CREB signaling pathway. This activator promotes neuronal proliferation, induces differentiation of Neuro-2a cells into neuron-like cells, and facilitates the axon-dendrite polarization in primary hippocampal neurons by upregulating brain-derived neurotrophic factor. It is particularly relevant for research into vascular dementia (VaD).
  29. PI3K/AKT Inhibitor

    PI3K/AKT-IN-1 is a potent dual inhibitor of the PI3K/AKT signaling pathway, exhibiting IC50 values of 6.99 μM for PI3Kγ, 4.01 μM for PI3Kδ, and 3.36 μM for AKT. This compound demonstrates significant anticancer activity by disrupting the PI3K/AKT axis, leading to the induction of caspase-3 dependent apoptosis. It serves as a valuable tool for research in cancer biology and therapeutic development targeting the PI3K/AKT pathway.
  30. AKT PROTAC Degrader

    MS21 is a potent AKT PROTAC degrader designed to selectively target and degrade AKT proteins. This compound effectively inhibits mutations within the PI3K/PTEN pathway, leading to suppressed tumor cell proliferation and induction of cell cycle arrest. MS21 demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development.
  31. PROTAC AKT Degrader

    MS170 is a highly selective PROTAC degrader targeting the AKT isoforms. With a DC50 value of 32 nM, MS170 effectively depletes total AKT (T-AKT) in cellular assays. It demonstrates strong binding affinity for AKT1, AKT2, and AKT3, with dissociation constants (Kd) of 1.3 nM, 77 nM, and 6.5 nM, respectively. This compound is suitable for research applications investigating AKT-related signaling pathways and therapeutic interventions in cancer biology.
  32. Endogenous Metabolite

    Ergothioneine is an endogenous metabolite that acts as a potent antioxidant. It functions primarily as a specific inhibitor of p38 MAPK and Akt, which are critical signaling pathways involved in cellular stress responses. Ergothioneine is utilized in research focused on neuroprotection, cell apoptosis, and oxidative stress, making it a valuable compound for investigations into cellular resilience and health.
  33. Secondary Metabolite

    Atranorin is a secondary metabolite derived from lichens that acts as an AKT inhibitor. This compound demonstrates a wide range of biological activities, including antibacterial, anti-inflammatory, antioxidant, anti-glycation, analgesic, and anti-tumor effects. Notably, Atranorin has IC50 values of 117 μM for scavenging DPPH free radicals and less than 10 μM for ABTS radicals, highlighting its potent antioxidant capacity. Additionally, Atranorin promotes wound healing and can be utilized in research focused on myelodysplastic syndromes, tumors, and various inflammatory conditions.
  34. Anti-Insect Agent

    Methyl Eugenol is an anti-insect agent primarily effective against the oriental fruit fly (Bactrocera dorsalis). In addition to its insecticidal properties, Methyl Eugenol exhibits anti-cancer and anti-inflammatory activities, making it a versatile compound for biological research. It has been shown to induce autophagy in cells and can be utilized in studies related to intestinal ischemia/reperfusion injury.
  35. Iron Chelator

    Deferoxamine (Deferoxamine B) is an iron chelator (binds to Fe(III) and many other metal cations), is widely used to reduce iron accumulation and deposition in tissues. Deferoxamine upregulates HIF-1α levels with good antioxidant activity. Deferoxamine also shows anti-proliferative activity, can induce apoptosis and autophagy in cancer cells. Deferoxamine can be used in studies of diabetes, neurodegenerative diseases as well as anti-cancer and anti-COVID-19.
  36. AMPK Agonist

    10-Gingerol is an AMPK agonist derived from ginger oleoresin, exhibiting notable anti-inflammatory, antioxidant, and anti-proliferative properties. It effectively suppresses neointimal hyperplasia and inhibits the proliferation of vascular smooth muscle cells. Demonstrating significant radical scavenging activities, 10-Gingerol has IC50 values of 10.47 μM against DPPH, 1.68 μM against superoxide, and 1.35 μM against hydroxyl radicals. This compound also inhibits MDA-MB-231 tumor cell line proliferation with an IC50 of 12.1 μM, while targeting the PI3K/Akt signaling pathway to suppress proliferation, migration, invasion, and promote apoptosis. It holds potential for research applications in ulcerative colitis.
  37. PPAR Activator

    Bilobetin acts as a PPARα activator, enhancing lipid metabolism and insulin sensitivity. It effectively reduces blood lipid levels by promoting hepatic lipid uptake and oxidation, while decreasing triglyceride secretion and accumulation in tissues. Additionally, Bilobetin stimulates the phosphorylation and nuclear translocation of PPARα, resulting in increased cAMP levels and PKA activity. This compound is significant for research in metabolic disorders, particularly those related to insulin resistance and lipid regulation.
  38. Glycosaminoglycan

    Hyaluronic acid sodium, also known as sodium hyaluronate, is a glycosaminoglycan that plays a crucial role in the extracellular matrix (ECM). This biopolymer is involved in key biological activities such as cell proliferation, tissue remodeling, and angiogenesis, particularly in the context of digestive cancers. Hyaluronic acid sodium is implicated in tumor cell growth and migration, and it activates the PI3K-Akt signaling pathway. This reagent can also be utilized in research related to joint diseases, wound healing, and as a drug delivery system to enhance the efficacy of therapeutics in cancer research.
  39. Akt Allosteric Inhibitor

    AKT-IN-28 is an allosteric inhibitor of Akt, a key protein involved in cell survival and metabolism. It exhibits a binding affinity with a Kd of 2.07 μM and demonstrates the ability to significantly inhibit Akt activity. This compound induces apoptosis, arrests the cell cycle in the G2/M phase, and suppresses proliferation, migration, and metabolic processes in KRAS mutant colorectal cancer cells, making it a valuable tool for cancer research applications focused on targeting the Akt pathway.
  40. Akt1/Akt2 Inhibitor

    Akt1/Akt2-IN-2 is an allosteric dual inhibitor targeting Akt1 and Akt2, exhibiting IC50 values of 138 nM and 212 nM, respectively. This compound enhances caspase-3 activity and effectively reduces the viability of various tumor cell lines. Its application in cancer research highlights its potential for investigating therapeutic strategies that disrupt Akt-mediated signaling pathways.
  41. Akt Inhibitor

    2-Chlorophenoxazine is an Akt inhibitor with an IC50 value of 2-5 μM in vitro. This compound has been shown to induce apoptosis in various cancer cell lines. It is a valuable tool for research into cancerpathways and therapeutic strategies targeting Akt signaling.
  42. CIP2A and p-Akt Inhibitor

    PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities. PP2A Cancerous-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  43. AKT Inhibitor

    AKT-IN-14 free base is a highly potent inhibitor of the AKT family of serine/threonine kinases, demonstrating IC50 values of less than 0.01 nM, 1.06 nM, and 0.66 nM for AKT1, AKT2, and AKT3, respectively. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating the role of AKT signaling in tumor progression and therapeutic resistance.
  44. Akt Substrate

    AKTide-2T is a selective substrate for AKT, demonstrating competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. This peptide mimics the optimal phosphorylation sequence of Akt, effectively serving as an inhibitory agent due to the absence of Thr at the S22 position in the wildtype sequence. It is a valuable tool for studying AKT signaling pathways and their implications in various biological processes.
  45. Akt Inhibitor

    DETD-35 is a potent inhibitor of the Akt signaling pathway, with additional effects on MEK-ERK and STAT3 pathways. It induces apoptosis in cancer cells and decreases their resistance to Vemurafenib. DETD-35 demonstrates effective inhibitory activity against various melanoma cell lines, with IC50 values of 2.5 to 6.0 μM across wild-type and mutant strains. This compound is a valuable tool for investigating mechanisms of anti-melanoma therapies.
  46. AKT Inhibitor

    AKT-IN-26 (Compound 453) is an AKT inhibitor that binds to the Pleckstrin homology (PH) domain of AKT. AKT-IN-26 can be used in research related to AKT pathway-associated cell proliferation and cancer.
  47. PI3K/AKT Pathways Inhibitor

    Isocucurbitacin B selectively inhibits the PI3K/AKT signaling pathways, along with the MAPK and STAT3 pathways, demonstrating notable anti-cancer properties. This natural terpenoid, derived from Pedicellus melo, effectively suppresses cancer cell proliferation, migration, and invasion. Additionally, Isocucurbitacin B induces apoptosis and facilitates G2/M phase cell cycle arrest, while altering intracellular cholesterol and pH levels, and elevating intracellular calcium levels. It serves as a valuable reagent for research applications in cancer biology, particularly in the study of glioma.
  48. Akt Inhibitor

    AM-9635 is a selective Akt inhibitor that targets the PI3Kδ pathway. It demonstrates significant in vitro and in vivo efficacy, effectively inhibiting PI3Kδ-dependent B cell receptor-mediated AKT phosphorylation. This compound has been shown to suppress the production of specific IgG and IgM antibodies in a rat model immunized with Aplysia leocyanin (KLH), making it useful for research applications in immunology and cancer biology.
  49. Akt Inhibitor

    CCT129254 is a selective inhibitor of the Akt pathway, targeting the serine/threonine kinase Akt. This compound demonstrates significant reduction in melanoma cell motility in vivo, highlighting its potential utility in cancer research. CCT129254 may serve as a valuable tool for studying the role of Akt in tumor progression and therapeutic resistance.
  50. TrkA/Akt Inhibitor

    HS-345 is a selective inhibitor of the TrkA/Akt signaling pathway, demonstrating significant anti-cancer effects in pancreatic cancer models. It inhibits the growth and proliferation of pancreatic cancer cells while inducing apoptosis. Moreover, HS-345 disrupts angiogenesis by downregulating the expression of HIF-1α and VEGF. This compound shows potential as a valuable tool for research into pancreatic cancer therapies.

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